CN113166206A - Glp-1受体拮抗剂 - Google Patents

Glp-1受体拮抗剂 Download PDF

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Publication number
CN113166206A
CN113166206A CN201980080295.9A CN201980080295A CN113166206A CN 113166206 A CN113166206 A CN 113166206A CN 201980080295 A CN201980080295 A CN 201980080295A CN 113166206 A CN113166206 A CN 113166206A
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China
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compound
syndrome
group
ser
lysr
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Pending
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CN201980080295.9A
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English (en)
Chinese (zh)
Inventor
盖尔斯·艾伯特·布朗
迈尔斯·斯图尔特·康格里夫
康纳·斯库利
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Nxera Pharma UK Ltd
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Heptares Therapeutics Ltd
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Publication of CN113166206A publication Critical patent/CN113166206A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/605—Glucagons
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/001—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Endocrinology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Toxicology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201980080295.9A 2018-10-12 2019-10-14 Glp-1受体拮抗剂 Pending CN113166206A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1816639.7A GB201816639D0 (en) 2018-10-12 2018-10-12 GLP-1 Receptor Antagonist
GB1816639.7 2018-10-12
PCT/GB2019/052915 WO2020074927A2 (en) 2018-10-12 2019-10-14 Glp-1 receptor antagonists

Publications (1)

Publication Number Publication Date
CN113166206A true CN113166206A (zh) 2021-07-23

Family

ID=64397527

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980080295.9A Pending CN113166206A (zh) 2018-10-12 2019-10-14 Glp-1受体拮抗剂

Country Status (8)

Country Link
US (2) US12441777B2 (https=)
EP (1) EP3863661A2 (https=)
JP (1) JP7492507B2 (https=)
CN (1) CN113166206A (https=)
AU (1) AU2019358324B2 (https=)
CA (1) CA3115448A1 (https=)
GB (1) GB201816639D0 (https=)
WO (1) WO2020074927A2 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB202011604D0 (en) * 2020-07-27 2020-09-09 Heptares Therapeutics Ltd GLP-1 receptor antagonists
CA3204051A1 (en) 2021-01-20 2022-07-28 Brian Lian Compositions and methods for the treatment of metabolic and liver disorders
JP7642830B2 (ja) 2021-09-15 2025-03-10 バイキング・セラピューティクス・インコーポレイテッド 代謝及び肝臓障害の処置のための組成物及び方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2335739A1 (en) * 2008-09-20 2011-06-22 Kyoto University Molecular probe precursor for imaging of pancreatic islet, and use thereof
EP2474326A1 (en) * 2009-09-04 2012-07-11 Kyoto University Molecular probe for imaging islets of langerhans, and use therefore
US20180117122A1 (en) * 2015-05-22 2018-05-03 The BOT of The LeIand Stanford Junior University Treatment of post-bariatric hypoglycemia with exendin (9-39)

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7399489B2 (en) 1999-01-14 2008-07-15 Amylin Pharmaceuticals, Inc. Exendin analog formulations
CN100540565C (zh) 2005-01-14 2009-09-16 无锡宏创医药科技有限公司 修饰的Exendins及其应用
WO2007139941A2 (en) 2006-05-26 2007-12-06 Amylin Pharmaceuticals, Inc. Composition and methods for treatment of congestive heart failure
WO2010120476A2 (en) 2009-04-01 2010-10-21 Amylin Pharmaceuticals, Inc. N-terminus conformationally constrained glp-1 receptor agonist compounds
CN101870728A (zh) 2009-04-23 2010-10-27 派格生物医药(苏州)有限公司 新型Exendin变体及其缀合物
US9278146B2 (en) * 2010-10-08 2016-03-08 Kyoto University Peptide derivative and use of the same
CN102532301B (zh) * 2010-12-31 2014-09-03 上海医药工业研究院 一类新型的Exendin-4类似物及其制备方法
GB201315335D0 (en) * 2013-08-29 2013-10-09 Of Singapore Amino diacids containing peptide modifiers

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2335739A1 (en) * 2008-09-20 2011-06-22 Kyoto University Molecular probe precursor for imaging of pancreatic islet, and use thereof
EP2474326A1 (en) * 2009-09-04 2012-07-11 Kyoto University Molecular probe for imaging islets of langerhans, and use therefore
US20180117122A1 (en) * 2015-05-22 2018-05-03 The BOT of The LeIand Stanford Junior University Treatment of post-bariatric hypoglycemia with exendin (9-39)

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
CHAHRZAD MONTROSE-RAFIZADEH 等: "High Potency Antagonists of the Pancreatic Glucagon-like Peptide-1 Receptor", 《THE JOURNAL OF BIOLOGICAL CHEMISTRY》, vol. 272, no. 34, pages 21201, XP002247450, DOI: 10.1074/jbc.272.34.21201 *
HIROYUKI KIMURA 等: "Evaluation of 18 F-labeled exendin(9-39) derivatives targeting glucagon-like peptide-1 receptor for pancreatic b-cell imaging", 《BIOORGANIC & MEDICINAL CHEMISTRY》, vol. 26, pages 463, XP085324175, DOI: 10.1016/j.bmc.2017.12.007 *
STEFFEN RUNGE 等: "Differential Structural Properties ofGLP-1 and Exendin-4 Determine Their Relative Affinity for theGLP-1 Receptor N-Terminal Extracellular Domain", 《BIOCHEMISTRY》, vol. 46, no. 19, pages 1 *

Also Published As

Publication number Publication date
AU2019358324B2 (en) 2025-05-22
AU2019358324A1 (en) 2021-04-22
CA3115448A1 (en) 2020-04-16
JP7492507B2 (ja) 2024-05-29
US12441777B2 (en) 2025-10-14
US20250368709A1 (en) 2025-12-04
US20210355186A1 (en) 2021-11-18
GB201816639D0 (en) 2018-11-28
WO2020074927A2 (en) 2020-04-16
JP2022504798A (ja) 2022-01-13
WO2020074927A3 (en) 2020-12-17
EP3863661A2 (en) 2021-08-18

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Country or region after: Britain

Address after: Cambridge, County of Cambridge, UK

Applicant after: Nexla Pharmaceuticals UK Ltd.

Address before: Cambridge, County of Cambridge, UK

Applicant before: Heptares Therapeutics Ltd.

Country or region before: Britain